JP7358342B2 - 新規なグルタミンアンタゴニストおよびそれらの使用 - Google Patents

新規なグルタミンアンタゴニストおよびそれらの使用 Download PDF

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JP7358342B2
JP7358342B2 JP2020519241A JP2020519241A JP7358342B2 JP 7358342 B2 JP7358342 B2 JP 7358342B2 JP 2020519241 A JP2020519241 A JP 2020519241A JP 2020519241 A JP2020519241 A JP 2020519241A JP 7358342 B2 JP7358342 B2 JP 7358342B2
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pharmaceutical composition
compound
group
alkyl
cancer
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JP2020536867A (ja
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バーバラ スラッシャー
ラナ ライス
パヴェル マイヤー
ルーカス テノラ
カテリーナ ノヴォトナ
ジェシー アルト
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ザ・ジョンズ・ホプキンス・ユニバーシティー
ウスタヴ オルガニケー ケミエ アー バイオケミエ アーヴェー チェーエル ヴェー.ヴェー.イー.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C245/00Compounds containing chains of at least two nitrogen atoms with at least one nitrogen-to-nitrogen multiple bond
    • C07C245/12Diazo compounds, i.e. compounds having the free valencies of >N2 groups attached to the same carbon atom
    • C07C245/14Diazo compounds, i.e. compounds having the free valencies of >N2 groups attached to the same carbon atom having diazo groups bound to acyclic carbon atoms of a carbon skeleton
    • C07C245/18Diazo compounds, i.e. compounds having the free valencies of >N2 groups attached to the same carbon atom having diazo groups bound to acyclic carbon atoms of a carbon skeleton the carbon skeleton being further substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/72Hydrazones
    • C07C251/74Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C251/76Hydrazones having doubly-bound carbon atoms of hydrazone groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of a saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/32Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C271/34Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D209/20Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals substituted additionally by nitrogen atoms, e.g. tryptophane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/26Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06086Dipeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/02Ortho- or ortho- and peri-condensed systems
    • C07C2603/04Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18Fluorenes; Hydrogenated fluorenes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00Systems containing at least three condensed rings
    • C07C2603/56Ring systems containing bridged rings
    • C07C2603/58Ring systems containing bridged rings containing three rings
    • C07C2603/70Ring systems containing bridged rings containing three rings containing only six-membered rings
    • C07C2603/74Adamantanes

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2020519241A 2017-10-06 2018-10-05 新規なグルタミンアンタゴニストおよびそれらの使用 Active JP7358342B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762569118P 2017-10-06 2017-10-06
US62/569,118 2017-10-06
US201862728214P 2018-09-07 2018-09-07
US62/728,214 2018-09-07
PCT/US2018/054581 WO2019071110A1 (en) 2017-10-06 2018-10-05 NOVEL GLUTAMINE ANTAGONISTS AND USES THEREOF

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JP2020536867A JP2020536867A (ja) 2020-12-17
JP7358342B2 true JP7358342B2 (ja) 2023-10-10

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US (1) US12195419B2 (da)
EP (1) EP3692015B1 (da)
JP (1) JP7358342B2 (da)
CN (1) CN111566083A (da)
DK (1) DK3692015T3 (da)
ES (1) ES2930258T3 (da)
WO (1) WO2019071110A1 (da)

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CN110520118A (zh) 2017-02-01 2019-11-29 约翰斯霍普金斯大学 谷氨酰胺类似物的前药
US20210177841A1 (en) * 2017-11-03 2021-06-17 Calithera Biosciences, Inc. Conjoint therapy with glutaminase inhibitors
BR112021014112A2 (pt) * 2019-01-18 2021-10-13 Dracen Pharmaceuticals, Inc. Usos de composto pró-fármaco de don e inibidor de ponto de controle imunológico para tratar câncer, bem como composto e composição farmacêutica compreendendo o mesmo
JP2022519530A (ja) * 2019-02-11 2022-03-24 ドラセン ファーマシューティカルズ インコーポレイテッド L-ピログルタミン酸からdonプロドラッグを調製する方法
EP3924330A4 (en) 2019-02-11 2022-11-09 Dracen Pharmaceuticals, Inc. PROCESS FOR THE PREPARATION OF A DON-PRODRUGE FROM L-GLUTAMIC ACID
CA3133735A1 (en) * 2019-03-18 2020-09-24 Alteron Therapeutics, Inc. Modulators of tdp-43
WO2021239049A1 (en) * 2020-05-27 2021-12-02 Jacobio Pharmaceuticals Co., Ltd. Novel glutamine analogs
WO2022022612A1 (en) * 2020-07-29 2022-02-03 Jacobio Pharmaceuticals Co., Ltd. Novel glutamine analogs
CN116601140A (zh) 2020-10-02 2023-08-15 羿尊生物医药股份有限公司 用于皮下施用的包含(s)-2-((s)-2-乙酰氨基-3-(1h-吲哚-3-基)丙酰氨基)-6-重氮基-5-氧代己酸异丙酯的冻干组合物及其用途
AU2021361970A1 (en) * 2020-10-15 2023-06-15 Jacobio Pharmaceuticals Co., Ltd. Novel glutamine analogs
WO2022078462A1 (en) * 2020-10-15 2022-04-21 Jacobio Pharmaceuticals Co., Ltd. Novel glutamine analogs
WO2022232565A1 (en) * 2021-04-29 2022-11-03 The Johns Hopkins University Prodrugs of 6-diazo-5-oxo-l-norleucine
JP2025078888A (ja) * 2022-01-28 2025-05-21 国立大学法人富山大学 グルタミナーゼ阻害剤
TW202404938A (zh) * 2022-04-21 2024-02-01 大陸商北京加科思新藥研發有限公司 麩醯胺酸拮抗劑的多晶型及其用途
CN120265609A (zh) * 2022-11-02 2025-07-04 约翰霍普金斯大学 具有优先肿瘤递送的阿佐霉素前药

Citations (2)

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WO2017023774A1 (en) 2015-07-31 2017-02-09 The Johns Hopkins University Prodrugs of glutamine analogs
WO2017023787A1 (en) 2015-07-31 2017-02-09 The Johns Hopkins University Methods and compositions for treating metabolic reprogramming disorders

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US5158976A (en) * 1990-10-29 1992-10-27 The Children's Medical Center Corporation Controlling glutamine/glutamate related neuronal injury
US20060276438A1 (en) * 2004-10-04 2006-12-07 Natarajan Sethuraman Prevention and treatment of influenza with glutamine antagonist agents
US7585996B2 (en) 2006-09-15 2009-09-08 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
US8343477B2 (en) 2006-11-01 2013-01-01 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus
WO2009029729A1 (en) 2007-08-31 2009-03-05 Genelabs Technologies, Inc. Amino tricyclic-nucleoside compounds, compositions, and methods of use
WO2017023791A1 (en) 2015-07-31 2017-02-09 The Johns Hopkins University Glutamine antagonists for the treatment of cognitive deficits
US10842763B2 (en) 2015-07-31 2020-11-24 The Johns Hopkins University Methods for cancer and immunotherapy using prodrugs of glutamine analogs
PE20190258A1 (es) 2015-12-09 2019-02-25 Res Triangle Inst Antagonistas del receptor de la apelina (apj) mejorados y usos de los mismos
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WO2017023787A1 (en) 2015-07-31 2017-02-09 The Johns Hopkins University Methods and compositions for treating metabolic reprogramming disorders

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Publication number Publication date
ES2930258T3 (es) 2022-12-09
EP3692015A1 (en) 2020-08-12
DK3692015T3 (da) 2022-11-21
US20230009398A1 (en) 2023-01-12
CN111566083A (zh) 2020-08-21
WO2019071110A1 (en) 2019-04-11
US12195419B2 (en) 2025-01-14
EP3692015B1 (en) 2022-08-24
EP3692015A4 (en) 2021-06-30
JP2020536867A (ja) 2020-12-17

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